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五年一次的综述:抗疟药物的最新进展和发展

A Quinquennial Review on Recent Advancements and Developments in Search of Anti-malarial Agents.

机构信息

Department of Pharmaceutical Chemistry, L. M. College of Pharmacy, Navrangpura, Ahmedabad, Gujarat, 380 009, India.

Department of Pharmaceutical Chemistry, Institute of Pharmacy, Nirma University, Ahmedabad, Gujarat, 382 481, India.

出版信息

Curr Top Med Chem. 2023;23(9):753-790. doi: 10.2174/1568026623666230427115241.

Abstract

Malaria has been a major parasitic disease in tropical and subtropical regions and is estimated to kill between one and two million people (mainly children) every year. Novel anti-malarial agents are urgently needed to combat the malarial parasites enduring resistance to the current medications, leading to increased morbidity and mortality. The heterocycles, holding a prominent position in chemistry and found in both natural and synthetic sources, have shown several biological activities including anti-malarial activity. Towards this goal, several research groups have reported the design and development of novel and potential anti-malarial agents like artemisinin, benzimidazole, benzothiazole, chalcone, cyclopeptide, fosmidomycin, furan, indole oxadiazole, 2-oxindoles, peroxides, pyrazole, pyrazolines, pyridines, pyrimidine, pyrrolidine, quinazoline, quinazolinone, quinolone, quinoline, thiazole, triazole and other scaffolds acting against newly emerging anti-malarial targets. The present work reports the complete quinquennial coverage of anti-malarial agents reported during 2016-2020 with a view of providing the merits and demerits of reported anti-malarial scaffolds, structure-activity relationship, along with their in vitro/ in vivo/ in silico profiles to the medicinal chemists working in the field of design and discovery of novel anti-malarial agents.

摘要

疟疾一直是热带和亚热带地区的主要寄生虫病,据估计,每年有 100 万至 200 万人(主要是儿童)因此死亡。新型抗疟药物急需用于对抗对现有药物具有抗药性的疟原虫,从而导致发病率和死亡率上升。杂环化合物在化学中占有重要地位,存在于天然和合成来源中,具有多种生物活性,包括抗疟活性。为此,一些研究小组报告了几种新型潜在抗疟药物的设计和开发,如青蒿素、苯并咪唑、苯并噻唑、查耳酮、环肽、福米霉素、呋喃、吲哚恶二唑、2-氧吲哚、过氧化物、吡唑、吡唑啉、吡啶、嘧啶、吡咯烷、喹唑啉、喹唑啉酮、喹诺酮、喹啉、噻唑、三唑和其他针对新出现的抗疟靶点的支架。本工作报道了 2016-2020 年期间报道的抗疟药物的完整五年覆盖,旨在为从事新型抗疟药物设计和发现的药物化学家提供报告的抗疟支架的优缺点、构效关系以及它们的体外/体内/计算机研究概况。

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